Prothionamide - instructions for use, dose, side effects, contraindications

auxiliary substances (core): cellulose microcrystalline 58.5 mg, giprolose (hydroxypropyl cellulose) 8.0 mg, sodium carboxymethyl starch 12.0 mg, water 4.0 mg, povidone (polyvinylpyrrolidone) 14.0 mg, sodium stearyl fumarate 3.5 mg;

auxiliary substances (shell): hypromellose 5.95 mg, macrogol-4000 1.4 mg, titanium dioxide 2.5 mg, dye quinoline yellow 0.15 mg.

Description:

Round, biconvex tablets, covered with a film coating of yellow color. On the fracture, two layers are visible: a yellow core and a film shell.

Pharmacotherapeutic group:anti-tuberculosis drug

ATX: & nbsp

J.04.A.D.01 Prothionamide

Pharmacodynamics:

Anti-tuberculosis drug of the II series. It blocks the synthesis of mycolic acids, which are the most important structural component of the mycobacterium tuberculosis cell wall; has the properties of a nicotinic acid antagonist. In high concentrations, the synthesis of the protein of the microbial cell is disrupted. Has a bacteriostatic effect. Active, especially in an acidic environment, with respect to fast and slow breeding Mycobacterium tuberculosis, located outside and intracellularly. In the process of treatment, the resistance of microorganisms rapidly develops, complete cross-resistance to ethionamide is noted. It inhibits the development of resistance to other anti-tuberculosis drugs.

The use in combination with other anti-tuberculosis drugs reduces the likelihood of developing resistance.

Pharmacokinetics:

Prothionamide is rapidly absorbed in the gastrointestinal tract, reaching a maximum concentration in the blood plasma 2-3 hours after ingestion. Penetrates into healthy and pathologically altered tissues (tuberculosis foci, including encapsulated, caverns in the lungs, serous and purulent pleural effusion, cerebrospinal fluid during meningitis, penetrates the placental barrier).Metabolised in the liver (one of the metabolites - sulfoxide, has tuberculostatic activity). It is excreted mainly by the kidneys (15-20% unchanged).

Indications:

Treatment of all forms of tuberculosis (both pulmonary and extrapulmonary): infiltrative, ulcerative and exudative forms.

In the combination therapy with resistance of the pathogen to other anti-tuberculosis drugs (I series) or their intolerance.

Contraindications:

Hypersensitivity to the protionamide and / or other components of the drug, acute gastritis, peptic ulcer and duodenal ulcer, ulcerative colitis, cirrhosis and other liver diseases in the acute phase, acute hepatitis, chronic alcoholism, renal failure, epilepsy, psychosis, pregnancy, period breastfeeding, children's age (not recommended for children under 3 years old).

Carefully:

Diabetes mellitus, severe hepatic insufficiency, depression, central nervous system diseases, hemoptysis, coagulopathy.

Pregnancy and lactation:

In pregnancy, the use of the drug is contraindicated. Prothionamide penetrates the placenta.

For the duration of treatment, breastfeeding should be discontinued.

Dosing and Administration:

Inside, after eating.

The daily dose for adults is 0.5-1 g / day in 2-3 divided doses. Begin treatment with 250 mg / day, then increase the dose by 250 mg every other day.

In patients older than 60 years and with a body weight of less than 50 kg, the daily dose should not exceed 750 mg (250 mg 3 times per day).

Children older than 3 years - at a rate of 10-20 mg / kg per day. The maximum daily dose for children should not exceed 500 mg of protionamide.

Duration of treatment - 8-9 months.

Side effects:

From the side of the blood and lymphatic system: anemia, methemoglobinemia, hypoprothrombinemia and hypofibrinogenemia.

From the digestive system: loss of appetite, heartburn, abdominal pain, a feeling of heaviness in the stomach, diarrhea or constipation, flatulence, nausea, vomiting, dry mouth or hypersalivation, swelling of the parotid salivary glands, "metallic" taste in the mouth, stomatitis, cheilitis, glossitis, dysfunction liver, increased activity of "liver" transaminases, severe hepatitis with jaundice, hepatic insufficiency.

From the nervous system: insomnia, agitation, depression, anxiety, dizziness, drowsiness, headache,asthenia, peripheral polyneuropathy, optic neuritis, impaired concentration, confusion, psychosis, convulsions, attempts at suicide, paresthesia, ataxia.

On the part of the organs of vision: blurred vision, paralysis of the eye muscles and accommodation, visual impairment, including diplopia.

From the respiratory system: hemoptysis.

From the skin and subcutaneous fat: photodermatosis, acne, alopecia.

From the side of skeletal musculature and connective tissue: arthralgia, arthritis, myalgia, shoulder syndrome, manifested by aldystrophy.

From the side of the kidneys: urolithiasis.

From the organs of hearing: hearing loss, tinnitus.

From the cardiovascular system: tachycardia, orthostatic hypotension.

From the endocrine system: hypoglycemia in patients with diabetes mellitus, gynecomastia, dysmenorrhea, amenorrhea, hypothyroidism, decreased potency.

Allergic reactions: skin rash.

Other: pellagro-like reactions, weakness.

Overdose:

Symptoms: impaired liver function, encephalopathy, pellagrope-like skin reactions.

Treatment: withdrawal of the drug, symptomatic treatment.

Interaction:

Increases the toxic effect of alcohol.

When used concomitantly with other antituberculosis drugs, synergy is manifested in relation to the main action.

Isoniazid increases the concentration of protionamide in plasma.

When used simultaneously with hormonal contraceptives, the increase in the hepatotoxic effect of protionamide.

With simultaneous admission with isoniazid, rifampicin and pyrazinamide, the risk of hepatotoxicity increases, with cycloserine - seizures become more frequent.

During treatment in patients with diabetes should adjust the dose of insulin or oral hypoglycemic agents.

To reduce the risk of side effects, combined with the intake of vitamin B₆ in a dose of 150-300 mg / day.

Special instructions:

It is recommended to start the course after determining the bacteriological sensitivity and prescribe the dose on the basis of individual sensitivity and tolerability.

Before treatment, it is necessary to study the gastrointestinal tract and liver function. During treatment, the activity level of "hepatic" transaminases, gamma-glutamate transferase and alkaline phosphatase should be monitored monthly,patients with diabetes mellitus - regularly determine the concentration of glucose.

Skin reactions may be the first signs of pellagruide-like side effects. This should be regarded as the reason for the necessary withdrawal of the drug.

For the duration of treatment, one should refrain from using ethanol because of the danger of inhibiting the central nervous system (associated with increased toxic effect of ethanol).

Effect on the ability to drive transp. cf. and fur:

Given the profile of side effects (dizziness, drowsiness, vomiting and others), it is recommended during treatment to refrain from driving, from practicing other potentially dangerous activities that require increased concentration and speed of psychomotor reactions.

Form release / dosage:

Tablets coated with a film coating, 250.0 mg.

Packaging:

For 10, 20, 25, 30 or 50 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

10, 20, 25, 30, 40, 50, 60, 100 or 1000 tablets in a polymer can for medicines.

One bank or 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10 contour cell packs together with the instruction for use are placed in a cardboard box(pack).

Storage conditions:

In the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use the drug after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LP-002338

Date of registration:30.12.2013

The owner of the registration certificate:ATOLL, LLC ATOLL, LLC Russia

Manufacturer: & nbsp

OZONE, LLC Russia

Information update date: & nbsp09.09.2015

Illustrated instructions

Instructions

Prothionamide (Protionamide)